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21 Cards in this Set

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  • Back

In Michaelis-Menton kinetics, what is [S], V, Km, and Vmax?

[s] = concentration of the substrate


V = velocity


Km= Substrate concentration. concentration of the substrate that gets the reaction to half of Vmax.


Vmax= Directly proportional to the enzyme concentration (the enzyme available)

Enzymatic reactions that exhibit a sigmoid curve usually indicates...

cooperative kinetics

The higher the affinity for the enzyme...

the faster it reaches Vmax. Therefor the lower Km will be.


Competetive inhibitors affect _____ but not _____

Competetive inhibitors affect Km (by increasing it) but not Vmax

Non-competetive inhibitors affect ____but not____

Non-competetive inhibitors affect Vmax(by lowering it) but not Km.

What is the definition of volume of distrubution?

theoretical volume that the absorbed drug occupied in the plasma.

What characteristics do drug molecules need to have in order to reach a high Vd?

Small


hydrophilic (ECF) or lipophilic (all tissues, especially if bound to tissue protein)

What is the clearance formula?

CL= rate of elimination of drug/plasma concentration= Vd x Ke(elimination constant)

What is the definition of clearance?

The volume of plasma cleared of drug per unit time.

What is the definition of Half Life?

time required to eliminate 50% of the drug.

What does Efficacy mean?

Maximal effect a drug can produce.


Does not have to do with potency.

If drug A (20mg) and drug B(10mg) are given at the same time and at 4 hours they have both achieved the same effect, what does this mean?

That drug B is more potent

If drug A (20mg) and drug B(20mg) are given at the same time and at 4 hours drug A caused more effect than drug B, you can infer that....

Drug A is more efficacious

What type of drugs have high efficacy?

antibiotics, antihistamines, decongestants

What types of drugs have high potency?

chemotherapeutic, antihypertensive, lipid lowering drugs

How does a competitive antagonist affect the potency/efficacy?

Shifts curve to the right (lowers potency bc you have to give more dose).



No change in efficacy. (bc the effect is the same)


How does a noncompetitive antagonist/reversible competitive antagonist affect the potency/efficacy?

Shifts curve down (lowers efficacy bc it does not reach maximum effect)



No change in potency (bc the dose is the same)

How does a partial agonist affect the potency/efficacy?

Lower maximum effect, and the potency is an independent value.


At higher therapeutic index....

The safer the drug is.



This happens if the lethal dose is high or the effective dose is low


Some drugs with low therapeutic index are..

Seizure drugs


Lithium


Digoxin


Warfarin


the higher the therapeutic window ...

You can give the medication frequently without risk o